Compound and pharmaceutical composition for treatment of...

C - Chemistry – Metallurgy – 07 – G

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C07G 99/00 (2009.01) C07G 17/00 (2006.01) A61K 35/78 (1990.01)

Patent

CA 2100781

2100781 9212720 PCTABS00014 A compound for the treatment of calcium oxalate kidney stone disease which can be extracted and purified from leaves of the plant Eriobotrya japonica is disclosed. The compound has the following characteristics: inhibits calcium oxalate crystal growth in vitro, inhibits renal calcium oxalate crystal deposition in rats which are fed ethylene glycol, causes rats which are fed ethylene glycol and said compound to excrete less oxalate in their urine as compared to rats which are fed ethylene glycol without said compound, shows little or no loss in activity when exposed to an aqueous solution of pH 1.5 for 14 hours, shows increased activity when exposed to an aqueous solution of pH 12.7 for 15 hours, is polyanionic, is stable when heated in an aqueous solution (at pH of extract) at 98 ·C for 3 hours, water-soluble, insoluble in heptane, hexane, chloroform/methanol mix, diethyl ether, and ethanol/aqueous mix, binds to DEAE-A-25 Sephadex at pH 8.6 and is eluted from the DEAE-A-25 Sephadex with 2 M NaCl. The present invention is also directed to a method for the treatment of calcium oxalate stone disease wherein the compound is administered, preferably for a prolonged period of time, to a patient suffering from or prone to calcium oxalate stone disease.

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